Kocurin
(Synonyms: Baringolin, PM181104) 目录号 : GC47530
A peptide antibiotic
Cas No.:1374772-61-8
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >70.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Kocurin is a thiazolyl peptide originally isolated from K. palustris and has antibiotic activity.1 It is active against methicillin-resistant S. aureus (MRSA; MIC = 0.25 µg/ml), as well as B. subtilis and E. faecium in a solid agar test when used at a concentration of 8 µg/ml. Kocurin is also active against E. faecium, E. faecalis, S. epidermidis, and clinical isolates of vancomycin-resistant enterococci (MICs = 0.004-1.025 µg/ml).2 In vivo, kocurin (2.5, 5, and 10 mg/ml) increases survival in a mouse model of E. faecium-induced septicemia. It decreases the number of colony forming units (CFUs) in a mouse model of MRSA lung infection.
1.Martin, J., da S. Sousa, T., Crespo, G., et al.Kocurin, the true structure of PM181104, an anti-methicillin-resistant Staphylococcus aureus (MRSA) thiazolyl peptide from the marine-derived bacterium Kocuria palustrisMar. Drugs11(2)387-398(2013) 2.Mahajan, G., Thomas, B., Parab, R., et al.In vitro and in vivo activities of antibiotic PM181104Antimicrob. Agents Chemother.57(11)5315-5319(2013)
| Cas No. | 1374772-61-8 | SDF | |
| 别名 | Baringolin, PM181104 | ||
| Canonical SMILES | [H][C@]1(CCCN1C([C@H](CC2=CC=C(O)C=C2)NC([C@]3([H])CSC([C@H](CC4=CC=CC=C4)NC5=O)=N3)=O)=O)C6=NC(C7=NC(C8=NC(C9=NC(C(NC(C(N[C@@H](C)C(N%10[C@H](C(NC(C(NC(C(N)=O)=C)=O)=C)=O)CCC%10)=O)=O)=C)=O)=CS9)=CC=C8C%11=NC(C(N[C@@H](CC(N)=O)C%12=NC5=CS%12)=O)=C(C)O%11)=CS7)=CS6 | ||
| 分子式 | C69H66N18O13S5 | 分子量 | 1515.7 |
| 溶解度 | Dichloromethane: soluble,DMSO: soluble,Ethanol: soluble,Methanol: soluble | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 0.6598 mL | 3.2988 mL | 6.5976 mL |
| 5 mM | 0.132 mL | 0.6598 mL | 1.3195 mL |
| 10 mM | 0.066 mL | 0.3299 mL | 0.6598 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Secondary Metabolites of Actinomycetes and their Antibacterial, Antifungal and Antiviral Properties
Pol J Microbiol 2018;67(3):259-272.PMID:30451442DOI:10.21307/pjm-2018-048.
The growing resistance of microorganisms towards antibiotics has become a serious global problem. Therapeutics with novel chemical scaffolds and/or mechanisms of action are urgently needed to combat infections caused by multidrug resistant pathogens, including bacteria, fungi and viruses. Development of novel antimicrobial agents is still highly dependent on the discovery of new natural products. At present, most antimicrobial drugs used in medicine are of natural origin. Among the natural producers of bioactive substances, Actinobacteria continue to be an important source of novel secondary metabolites for drug application. In this review, the authors report on the bioactive antimicrobial secondary metabolites of Actinobacteria that were described between 2011 and April 2018. Special attention is paid to the chemical scaffolds, biological activities and origin of these novel antibacterial, antifungal and antiviral compounds. Arenimycin C, chromopeptide lactone RSP 01, Kocurin, macrolactins A1 and B1, chaxamycin D as well as anthracimycin are regarded as the most effective compounds with antibacterial activity. In turn, the highest potency among selected antifungal compounds is exhibited by enduspeptide B, neomaclafungins A-I and kribelloside D, while ahmpatinin i Bu, antimycin A1a, and pentapeptide 4862F are recognized as the strongest antiviral agents.
Kocurin, the true structure of PM181104, an anti-methicillin-resistant Staphylococcus aureus (MRSA) thiazolyl peptide from the marine-derived bacterium Kocuria palustris
Mar Drugs 2013 Feb 4;11(2):387-98.PMID:23380989DOI:10.3390/md11020387.
A new thiazolyl peptide, Kocurin (1), was isolated from culture broths of a marine-derived Kocuria palustris. Its structural elucidation was accomplished using a combination of spectroscopic and chemical methods, including HRMS, extensive 1D and 2D NMR analysis, MS/MS fragmentation, and chemical degradation and Marfey's analysis of the resulting amino acid residues. The structure herein reported corrects that previously assigned to PM181104 (3). Kocurin displayed activity against methicillin-resistant Staphylococcus aureus (MRSA), with MIC values in the submicromolar range.
Identification and heterologous expression of the Kocurin biosynthetic gene cluster
Microbiology (Reading) 2017 Oct;163(10):1409-1414.PMID:28942758DOI:10.1099/mic.0.000538.
The antibiotically bioactive thiopeptide compound Kocurin was identified in extracts from a newly isolated Kocuria rosea strain. The axenic strain was retrieved from a soil sample of the intertidal area at the Paracas National Park, Peru. The genetic basis of this promising natural product with activity against methicillin-resistant Staphylococcus aureus (MRSA) strains was revealed by comparative genome analysis of this new isolate and other reported thiopeptide producer strains. The functionality of the predicted gene locus was experimentally proven by heterologous expression in Streptomyces coelicolor M1146. Expression of the gene cluster under the control of a constitutive promoter enabled the transgenic strain to produce Kocurin in selected media. The Kocurin biosynthetic gene cluster comprises nine open reading frames and spans around 12 kbp of the genome.
Bioprospecting Sponge-Associated Microbes for Antimicrobial Compounds
Mar Drugs 2016 May 2;14(5):87.PMID:27144573DOI:10.3390/md14050087.
Sponges are the most prolific marine organisms with respect to their arsenal of bioactive compounds including antimicrobials. However, the majority of these substances are probably not produced by the sponge itself, but rather by bacteria or fungi that are associated with their host. This review for the first time provides a comprehensive overview of antimicrobial compounds that are known to be produced by sponge-associated microbes. We discuss the current state-of-the-art by grouping the bioactive compounds produced by sponge-associated microorganisms in four categories: antiviral, antibacterial, antifungal and antiprotozoal compounds. Based on in vitro activity tests, identified targets of potent antimicrobial substances derived from sponge-associated microbes include: human immunodeficiency virus 1 (HIV-1) (2-undecyl-4-quinolone, sorbicillactone A and chartarutine B); influenza A (H1N1) virus (truncateol M); nosocomial Gram positive bacteria (thiopeptide YM-266183, YM-266184, mayamycin and Kocurin); Escherichia coli (sydonic acid), Chlamydia trachomatis (naphthacene glycoside SF2446A2); Plasmodium spp. (manzamine A and quinolone 1); Leishmania donovani (manzamine A and valinomycin); Trypanosoma brucei (valinomycin and staurosporine); Candida albicans and dermatophytic fungi (saadamycin, 5,7-dimethoxy-4-p-methoxylphenylcoumarin and YM-202204). Thirty-five bacterial and 12 fungal genera associated with sponges that produce antimicrobials were identified, with Streptomyces, Pseudovibrio, Bacillus, Aspergillus and Penicillium as the prominent producers of antimicrobial compounds. Furthemore culture-independent approaches to more comprehensively exploit the genetic richness of antimicrobial compound-producing pathways from sponge-associated bacteria are addressed.
Antibacterial Compounds from Marine Bacteria, 2010-2015
J Nat Prod 2017 Apr 28;80(4):1215-1228.PMID:28362500DOI:10.1021/acs.jnatprod.6b00235.
This review summarizes the reports on antibacterial compounds that have been obtained from marine-derived bacteria during the period 2010-2015. Over 50 active compounds were isolated during this period, most of which (69%) were obtained from Actinobacteria. Several compounds were already known, such as etamycin A (11) and nosiheptide (65), and new experiments with them showed some previously undetected antibacterial activities, highlighting the fact that known natural products may be an important source of new antibacterial leads. New broad-spectrum antibacterial compounds were reported with activity against antibiotic resistant Gram-positive and Gram-negative bacteria. Anthracimycin (33), Kocurin (66), gageotetrins A-C (72-74), and gageomacrolactins 1-3 (86-88) are examples of compounds that display promising properties and could be leads to new antibiotics. A number of microbes produced mixtures of metabolites sharing similar chemical scaffolds, and structure-activity relationships are discussed.